ReviewACS pharmacology & translational science2018
Beyond Glucagon-like Peptide-1: Is G-Protein Coupled Receptor Polypharmacology the Path Forward to Treating Metabolic Diseases?
Review in ACS pharmacology & translational science, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
19 citing papers in PubMed, 30 citations in OpenAlex.
- Tirzepatide retention in iWAT with mesoporous polydopamine encapsulation enhances weight loss through leptin receptor signaling.Journal of advanced research · 2026Article
- Adverse events associated with tirzepatide: a focus on subgroup-specific differences.BMC pharmacology & toxicology · 2026Article
- The GIP receptor activates futile calcium cycling in white adipose tissue to increase energy expenditure and drive weight loss in mice.Cell metabolism · 2025Article
- Review
- Evaluating glucose-dependent insulinotropic polypeptide and glucagon as key regulators of insulin secretion in the pancreatic islet.American journal of physiology. Endocrinology and metabolism · 2024Review
- Article
- Reduced GLP-1R availability in the caudate nucleus with Alzheimer's disease.Frontiers in aging neuroscience · 2024Article
- The Potential Utility of Tirzepatide for the Management of Polycystic Ovary Syndrome.Journal of clinical medicine · 2023Review
- Diabetes and its Complications.ACS pharmacology & translational science · 2022Article
- Review
- GIPR agonism mediates weight-independent insulin sensitization by tirzepatide in obese mice.The Journal of clinical investigation · 2021Article
- GPR120/FFAR4 Pharmacology: Focus on Agonists in Type 2 Diabetes Mellitus Drug Discovery.Journal of medicinal chemistry · 2021Article
- Discovery of small molecule positive allosteric modulators of the secretin receptor.Biochemical pharmacology · 2021Article
- Therapeutic Peptides Targeting PPI in Clinical Development: Overview, Mechanism of Action and Perspectives.Frontiers in molecular biosciences · 2021Review
- Development of a Testing Funnel for Identification of Small-Molecule Modulators Targeting Secretin Receptors.SLAS discovery : advancing life sciences R & D · 2021Article
- Proglucagon-Derived Peptides as Therapeutics.Frontiers in endocrinology · 2021Review
- Article
- Leveraging the Gut to Treat Metabolic Disease.Cell metabolism · 2020Review
- Incretin Mimetics as Rational Candidates for the Treatment of Traumatic Brain Injury.ACS pharmacology & translational science · 2019Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The glucagon-like peptide-1 receptor (GLP-1R) is a class B G-protein coupled receptor (GPCR) that has proven to be an effective target for developing medicines that treat type 2 diabetes mellitus (T2DM). GLP-1R agonists improve T2DM by enhancing glucose-stimulated insulin secretion, delaying gastric transit, decreasing glucagon levels, and reducing body weight due to anorexigenic actions. The therapeutic successes of these agents helped inspire the design of new multifunctional molecules that are GLP-1R agonists but also activate receptors linked to pathways that enhance insulin sensitization and/or energy expenditure. Herein, these agents are discussed in the context of polypharmacological approaches that may enable even further improvement in treatment outcomes. Moreover, we revisit classical polypharmaceutical GPCR approaches and how they may be utilized for treatment of T2DM. To determine optimal combination regimens, changes in drug discovery practices are likely needed because compensatory mechanisms appear to underlie progression of T2DM and limit the ability of current therapies to induce disease regression or remission.
Identifiers
What Socratic holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.